CAS NO: | 2081093-21-0 |
包装 | 价格(元) |
100mg | 电议 |
250mg | 电议 |
500mg | 电议 |
生物活性 | CHMFL-ABL/KIT-155 (CHMFL-ABL-KIT-155; compound 34) is a highly potent and orally activetype II ABL/c-KITdual kinase inhibitor (IC50s of 46 nM and 75 nM, respectively), and it also presents significant inhibitory activities to BLK (IC50=81 nM), CSF1R (IC50=227 nM),DDR1(IC50=116 nM),DDR2(IC50=325 nM), LCK (IC50=12 nM) andPDGFRβ(IC50=80 nM) kinases. CHMFL-ABL/KIT-155 (CHMFL-ABL-KIT-155) arrests cell cycle progression and inducesapoptosis[1]. |
IC50& Target | IC50: 46 nM (type II ABL), 75 nM (c-KIT), 81 nM (BLK), 227 nM (CSF1R), 116 nM (DDR1), 325 nM (DDR2), 12 nM (LCK), 80 nM (PDGFRβ)[1] |
体外研究 (In Vitro) | CHMFL-ABL/KIT-155 (CHMFL-ABL-KIT-155) exhibits anti-proliferation activities in the BCR-ABL dependent CML cancer cell lines such as K562 (GI50: 0.027 μM), MEG-01 (GI50: 0.02 μM), and KU812 (GI50: 0.056 μM). It also potently inhibits the growth of c-KIT dependent GISTs cancer cell lines including GIST-T1 (GI50: 0.023 μM), GIST-882 (GI50: 0.095 μM) but not c-KIT independent GIST-48B (GI50: 3.96 μM)[1]. |
体内研究 (In Vivo) | CHMFL-ABL/KIT-155 (CHMFL-ABL-KIT-155) (25-100 mg/kg; p.o.; once daily for 28 days) shows dose-dependent tumor progression suppression without apparent toxicity in female nu/nu mice bearing established K562 tumor xenografts[1]. |
分子量 | 609.68 |
Formula | C33H38F3N5O3 |
CAS 号 | 2081093-21-0 |
运输条件 | Room temperature in continental US; may vary elsewhere. |
储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |